Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.64 extracted from

  • Roy, J.; Fournier, M.A.; Maltais, R.; Kenmogne, L.C.; Poirier, D.
    Reprint of in vitro and in vivo evaluation of a 3beta-androsterone derivative as inhibitor of 17beta-hydroxysteroid dehydrogenase type 3 (2015), J. Steroid Biochem. Mol. Biol., 153, 170-178.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene HSD17B3, recombinant expression in HEK-293 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3alpha,5alpha)-3-[(2,5-dimethyl-4-{[2-(trifluoromethyl)phenyl]sulfonyl}piperazin-1-yl)methyl]-3-hydroxyandrostan-17-one the inhibitor RM-532-105 seems to have difficulties in penetrating inside the testis and is concentrated in the testicular capsule. Therefore it is unable to inhibit the 17bets-HSD3 located inside the testis. At a higher concentration, RM-532-105 significantly decreases the level of testosterone and dihydrotestosterone in rat plasma, in vivo effects of the inhibitor in testis and plasma, detailed overview Rattus norvegicus
1-[(3R,5S,8R,9S,10S,13S,14S)-10,13-dimethyl-2',17-dioxohexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-3,5'-[1,3]oxazolidin]-3'-yl]-3-(morpholin-4-yl)propan-2-yl cyclohexanecarboxylate
-
Homo sapiens
RM-532-105
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
testosterone + NADP+ Rattus norvegicus
-
androstenedione + NADPH + H+
-
?
testosterone + NADP+ Homo sapiens
-
androstenedione + NADPH + H+
-
?
testosterone + NADP+ Rattus norvegicus Sprague-Dawley
-
androstenedione + NADPH + H+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P37058
-
-
Rattus norvegicus O54939
-
-
Rattus norvegicus Sprague-Dawley O54939
-
-

Source Tissue

Source Tissue Comment Organism Textmining
testis
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
testosterone + NADP+
-
Rattus norvegicus androstenedione + NADPH + H+
-
?
testosterone + NADP+
-
Homo sapiens androstenedione + NADPH + H+
-
?
testosterone + NADP+
-
Rattus norvegicus Sprague-Dawley androstenedione + NADPH + H+
-
?

Synonyms

Synonyms Comment Organism
17beta-HSD3
-
Rattus norvegicus
17beta-HSD3
-
Homo sapiens
17beta-hydroxysteroid dehydrogenase type 3
-
Rattus norvegicus
17beta-hydroxysteroid dehydrogenase type 3
-
Homo sapiens
HSD17B3
-
Rattus norvegicus
HSD17B3
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Rattus norvegicus
NADP+
-
Homo sapiens
NADPH
-
Rattus norvegicus
NADPH
-
Homo sapiens

General Information

General Information Comment Organism
metabolism the enzyme catalyzes the last step in the biosynthesis of the potent androgen testosterone (T), by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor Rattus norvegicus
metabolism the enzyme catalyzes the last step in the biosynthesis of the potent androgen testosterone (T), by stereoselectively reducing the C17 ketone of 4-androstene-3,17-dione (4-dione), with NADPH as cofactor Homo sapiens